Social scientists recognize that over population is one of the most serious problems which mankind must face and solve. As an example, in the United States the Department of Health, Education and Welfare released statistics recently which showed that 3.3 million babies were born in the United States in 1977, up 5% from the previous year. This marked an increase in the nation's birth rate for the first time since 1970. (1) The problem is even more critical in underdeveloped countries.
In order to control our increasing world population, there exists a myriad of contraceptive devices to prevent unwanted pregnancy.
Each method attempts to achieve a contraceptive possessing the qualities of simplicity, acceptability, efficacy, nontoxicity and absence of adverse side effects. One class of such measures are mechanical contraceptives, such as the diaphragm, which are inserted into the vagina to completely occlude the orifice of the cervix, thus obstructing the migration of spermatozoa upward into the fallopian tubes. Such contraceptives have serious application problems due to the wide variation in size and geometry of the vaginal canal and the cervical opening. These devices often require special insertion instruments and careful fitting, usually by a trained physician. Furthermore, since trained help in application is often necessary, these devices are ill-suited for the underdeveloped countries where they are needed most.
Chemical or spermicidal contraceptives are another well known method for attempting to prevent pregnancy. These devices consist of a carrier agent such as jellies and creams which provide partial obstruction of the cervix and in addition contain nontoxic chemical agents that immobilize sperm. The creams and jellies can be inserted high into the vagina with an applicator or can be encapsulated as capsules or suppositories. Capsules or suppositories are placed in the vagina shortly before coitus to allow sufficient time for them to melt and disperse their active ingredients. However, the use of these devices have resulted in unwanted pregnancies because the spermicidal material is not held for a sufficient length of time (which may be several hours) in the desired location in relation to the cervical opening. As a result of this inability to be effective alone, creams and jellies are often used in conjunction with other contraceptive devices. In addition, suppositories require skill in positioning the device in the depth of the vagina in order to prevent flow back out the vaginal opening.
Another type of mechanical device is the condom, a rubber device that surrounds the penis and contains the sperm after ejaculation. This widely used device suffers from an unnatural or desensitizing feeling to the male and female. In addition, the possibility of a perforation in the sheath and the problem of disposing of spent condoms, make the device less than the ultimate answer to unwanted pregnancy.
Recently, oral contraceptives have gained prominence. The "pill" is a female contraceptive which works by suppressing ovulation. One type of "pill" contains a combination of estrogen and progestogen. The Food and Drug Administration has recently published a brochure which reports that estrogen causes cancer in some animals, but studies have not confirmed that it causes cancer in humans. This brochure also states that the pill doubles a woman's change of having a heart attack as well as increasing the risk of other circulatory problems.
Risk of heart attack is further increased if the woman is a smoker. Pill users who smoke are three times more likely to die of a heart attack than nonsmokers on the pill and ten times more likely than nonsmokers who do not use the pill. (2)
The pill should not be taken by females who have certain ailments. In addition, undesirable side effects will sometimes occur when the female first takes the oral contraceptive. These include nausea and vomiting, increase in breast tenderness and engorgement, accentuation of acne, fluid retention, weight gain, increased vaginal discharge and breakthrough bleeding. Finally, there is documentation to the effect that the risk of death to the user may be on the order of 3 per 100,000. (3)
Given these problems with an oral female contraceptive, much pharmacological research has been focused recently upon producing male oral contraceptives. Alkylating agents and hormones to regulate spermatogenesis and thereby bring about a temporary or controlled sterility have been the subject of experimentation. However, alkylating agents are considered dangerous due to possible irreversible side effects and toxicity. Many unanswered questions remain with the use of hormones also. (4)
Due to the above deficiencies in prior contraceptive methods, recently there has been an attempt to begin discovering new fertility-control agents developed from plant extracts. In the January, 1978, issue of PHARMACEUTICAL TECHNOLOGY, the editors write that:
"In light of evidence that primitive people in certain parts of the world have been able to limit population growth by using plant extracts, the World Health Organization has approved an international program to find new fertility-regulating agents in plants. In 1978, the Department of Pharmacognosy and Pharmacology of the College of Pharmacy at the University of Illinois Medical Center, along with centers in London, Brazil, Hong Kong, South Korea, and Ceylon, will receive funds from WHO for this purpose.
Professor Norman R. Farnsworth, Ph.D., head of the Pharmacognosy and Pharmacology Department, stresses that plants are a key ingredient in our health-care system: at least 25% of all prescriptions dispensed by community pharmacies contain active principles still extracted from plants. `Most of these plant drugs,` he says, `have been discovered by scientists studying folklore uses of plants.` Other University of Illinois projects involve studying published articles on plants for new sources of drugs to treat cancer, pain and high blood pressure."
The invention disclosed is an oral contraceptive formulation which will obviate many of the deficiencies in the prior art. It is the first male oral contraceptive which has proven effectiveness by providing a carefully controllable, temporary sterility, and yet is simple, completely nontoxic, and possesses no side effects.